SML4294

SBI-115

≥98% (HPLC), powder, TGR5/GPBAR1 antagonist

• Synonim(y): 3-Methylphenyl 5-chloro-2-(ethylsulfonyl)-4-pyrimidinecarboxylate, m-tolyl 5-chloro-2-(ethylsulfonyl) pyrimidine-4-carboxylate, SBI-115, TGR5 Antagonist, SBI115, SBI 115
• Wzór empiryczny (zapis Hilla): C₁₄H₁₃ClN₂O₄S
• Numer CAS: 882366-16-7
• Masa cząsteczkowa: 340.78
• Assay: ≥98% (HPLC)
• Form: powder

Właściwości

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: -10 to -25°C

Opis

Application

SBI-115 may be used in cell proliferation and cyclic adenosine monophosphate (cAMP) assay to determine its effects on rodents with polycystic liver diseases and, to explore the mechanisms of TGR5 in inhibiting NLR family pyrin domain containing 3 (NLRP3) inflammasome under inflammatory conditions.

Biochem/physiol Actions

SBI-115, a specific TGR5/GPBAR1 antagonist, blocks agonist activation, inhibiting TGR5-Gαs-cAMP signaling and reducing intracellular cAMP in cystic cholangiocytes. This antagonism dose-dependently inhibits agonist-induced proliferation and reduces 3D cholangiocyte spheroid growth in vitro, enabling SBI-115 to attenuate Polycystic Liver Disease (PLD) pathology by modulating cAMP. Beyond PLD, SBI-115′s TGR5 modulation impacts inflammation by offsetting bile acid suppression of IL-1β/NLRP3 in macrophages and influences macrophage M2 polarization in non-small cell lung cancer, promoting antitumor immunity in vitro. Additionally, SBI-115 (1 µM) elevates triglycerides and reduces P-PPARA in fatty-degenerated hepatocytes, implicating TGR5 in lipid metabolism.

Ta strona może zawierać tekst przetłumaczony maszynowo.

Informacja o środkach bezpieczeństwa

• Klasa składowania: 11 - Combustible Solids
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable